Pharmaceutical Tablets: Tablet Surface Preparation and Analysis Methods

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Pharmaceutical Technology, Manufacturing and Devices".

Deadline for manuscript submissions: closed (30 August 2023) | Viewed by 5103

Special Issue Editor

Bristol-Myers Squibb, New York, NY, USA
Interests: novel drug delivery

Special Issue Information

Dear Colleagues,

A tablet is a tablet-shaped or shaped tablet-shaped solid preparation that is uniformly mixed with drugs and excipients, after which it is compressed. Tablets are mainly oral tablets, buccal tablets, sublingual tablets, buccal patches, chewable tablets, dispersible tablets, effervescent tablets, vaginal tablets, immediate-release, sustained-release, or controlled-release tablets, and enteric-coated tablets. Some tablet manufacturing methods include boiling granulation, full powder direct compression, semi-film coating, new excipients, new processes, and production linkage. The advantages of tablets include the following: a. Generally, the dissolution rate and bioavailability of tablets are better than those of pills. b. The dose is accurate, the differences in drug contents in tablets are small, and the quality is stable. c. Protected by coating, they are less affected by light, air, moisture, etc. d They are more convenient to take, carry, and transport. E. Their production is mechanized, with large outputs, low costs, and easy-to-meet hygienic standards. The disadvantages are as follows: a. Some excipients need to be added to tablets, and after compression molding the dissolution rate is slower than that of powders and capsules, which sometimes affects their bioavailability. b. Children and comatose patients do not find them easy to swallow. c. The contents of tablets containing volatile components decrease when stored for a long time. Most of the tablets on the market will have a film coating that serves several purposes, including taste masking, dissolution modification, and protection of the API from air, moisture, and light. The photostability of film-coated tablets often depends on the thickness of the top coating on the tablet.

Dr. Anuji Abraham
Guest Editor

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Keywords

  • drug dissolution
  • coating
  • hot melt extrusion
  • matrix tablets
  • drug release
  • poorly soluble drug
  • solubility improvement
  • drug targeting
  • drug delivery systems

Published Papers (3 papers)

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Research

15 pages, 6561 KiB  
Article
Surface Engineering Methods for Powder Bed Printed Tablets to Optimize External Smoothness and Facilitate the Application of Different Coatings
by Khanh T. T. Nguyen, Daan Zillen, Franca F. M. van Heijningen, Kjeld J. C. van Bommel, Renz J. van Ee, Henderik W. Frijlink and Wouter L. J. Hinrichs
Pharmaceutics 2023, 15(9), 2193; https://doi.org/10.3390/pharmaceutics15092193 - 24 Aug 2023
Viewed by 716
Abstract
In a previous attempt to achieve ileo-colonic targeting of bovine intestinal alkaline phosphatase (BIAP), we applied a pH-dependent coating, the ColoPulse coating, directly on powder bed printed (PBP) tablets. However, the high surface roughness necessitated an additional sub-coating layer [Nguyen, K. T. T., [...] Read more.
In a previous attempt to achieve ileo-colonic targeting of bovine intestinal alkaline phosphatase (BIAP), we applied a pH-dependent coating, the ColoPulse coating, directly on powder bed printed (PBP) tablets. However, the high surface roughness necessitated an additional sub-coating layer [Nguyen, K. T. T., Pharmaceutics 2022]. In this study, we aimed to find a production method for PBP tablets containing BIAP that allows the direct application of coating systems. Alterations of the printing parameters, binder content, and printing layer height, when combined, were demonstrated to create visually less rough PBP tablets. The addition of ethanol vapor treatment further improved the surface’s smoothness significantly. These changes enabled the direct application of the ColoPulse, or enteric coating, without a sub-coating. In vitro release testing showed the desired ileo-colonic release or upper-intestinal release for ColoPulse or enteric-coated tablets, respectively. Tablets containing BIAP, encapsulated within an inulin glass, maintained a high enzymatic activity (over 95%) even after 2 months of storage at 2–8 °C. Importantly, the coating process did not affect the activity of BIAP. In this study, we demonstrate, for the first time, the successful production of PBP tablets with surfaces that are directly coatable with the ColoPulse coating while preserving the stability of the encapsulated biopharmaceutical, BIAP. Full article
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16 pages, 4180 KiB  
Article
The Influence of Wet Granulation Parameters on the Compaction Behavior and Tablet Strength of a Hydralazine Powder Mixture
by Oliver Macho, Ľudmila Gabrišová, Adam Guštafík, Kristian Jezso, Martin Juriga, Juraj Kabát and Jaroslav Blaško
Pharmaceutics 2023, 15(8), 2148; https://doi.org/10.3390/pharmaceutics15082148 - 16 Aug 2023
Cited by 1 | Viewed by 1205
Abstract
The aim of this paper was to describe the influence of high-shear wet granulation process parameters on tablet tensile strength and compaction behavior of a powder mixture and granules containing hydralazine. The hydralazine powder mixture and eight types of granules were compacted into [...] Read more.
The aim of this paper was to describe the influence of high-shear wet granulation process parameters on tablet tensile strength and compaction behavior of a powder mixture and granules containing hydralazine. The hydralazine powder mixture and eight types of granules were compacted into tablets and evaluated using the Heckel, Kawakita and Adams analyses. The granules were created using two types of granulation liquid (distilled water and aqueous solution of polyvinylpyrrolidone), at different impeller speeds (500 and 700 rpm) and with different wet massing times (without wet massing and for 2 min). Granulation resulted in improved compressibility, reduced dustiness and narrower particle-size distribution. A significant influence of wet massing time on parameters from the Kawakita and Adams analysis was found. Wet massing time had an equally significant effect on tablet tensile strength, regardless of the granulation liquid used. Granules formed with the same wet massing time showed the same trends in tabletability graphs. Tablets created using a single-tablet press (batch compaction) and an eccentric tablet press showed opposite values of tensile strength. Tablets from granules with a higher bulk density showed lower strength during batch compaction and, conversely, higher strength during eccentric tableting. Full article
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33 pages, 7309 KiB  
Article
Moisture Behavior of Pharmaceutical Powder during the Tableting Process
by Komlan Koumbogle, Ryan Gosselin, François Gitzhofer and Nicolas Abatzoglou
Pharmaceutics 2023, 15(6), 1652; https://doi.org/10.3390/pharmaceutics15061652 - 04 Jun 2023
Cited by 2 | Viewed by 2862
Abstract
The moisture content of pharmaceutical powder is a key parameter contributing to tablet sticking during the tableting process. This study investigates powder moisture behavior during the compaction phase of the tableting process. Finite element analysis software COMSOL Multiphysics® 5.6 was used to [...] Read more.
The moisture content of pharmaceutical powder is a key parameter contributing to tablet sticking during the tableting process. This study investigates powder moisture behavior during the compaction phase of the tableting process. Finite element analysis software COMSOL Multiphysics® 5.6 was used to simulate the compaction microcrystalline cellulose (VIVAPUR PH101) powder and predict temperature and moisture content distributions, as well as their evolution over time, during a single compaction. To validate the simulation, a near-infrared sensor and a thermal infrared camera were used to measure tablet surface temperature and surface moisture, respectively, just after ejection. The partial least squares regression (PLS) method was used to predict the surface moisture content of the ejected tablet. Thermal infrared camera images of the ejected tablet showed powder bed temperature increasing during compaction and a gradual rise in tablet temperature along with tableting runs. Simulation results showed that moisture evaporate from the compacted powder bed to the surrounding environment. The predicted surface moisture content of ejected tablets after compaction was higher compared to that of loose powder and decreased gradually as tableting runs increased. These observations suggest that the moisture evaporating from the powder bed accumulates at the interface between the punch and tablet surface. Evaporated water molecules can be physiosorbed on the punch surface and cause a capillary condensation locally at the punch and tablet interface during dwell time. Locally formed capillary bridge may induce a capillary force between tablet surface particles and the punch surface and cause the sticking. Full article
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